egfr-in-12

EGFR-IN-12 (EGFR Inhibitor) is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.

EGFR HER2-IN-12 (compound 14b) serves as a dual inhibitor targeting EGFR and HER2, demonstrating 81% and 51% inhibition respectively at a concentration of 10 μM. This compound exhibits minimal toxicity towards A431 and MDA-MB-361 cancer cells [1].

EGFR-IN-122 (compound Yfq07) serves as a potent inhibitor of EGFR. It effectively inhibits the proliferation of PC-9GR and HCC827GR cells.

EGFR-IN-127 is an ATP-competitive inhibitor targeting EGFR, with IC50 values of 136.3 nM for EGFRdel19 and 161.2 nM for EGFRdel19 T790M C797S. This compound holds potential for the study of non-small cell lung cancer (NSCLC).

EGFR-IN-123 (compound D06) is an effective EGFR inhibitor. It exhibits inhibitory activity against several cell lines including PC-9G, A549, A431, and HCT116, with IC50 values of 0.74, 1.36, 1.20, and 2.53 μM respectively.

EGFR-IN-126 (compound 9d) is an effective inhibitor of EGFR L858R T790M C797S, displaying an IC50 value of 0.005 μM. It exhibits antitumor activity both in vivo and in vitro.

EGFR-IN-124 (compound 10A) is an EGFR inhibitor with an IC50 value of 0.54 μM, utilized in cancer research.

EGFR-IN-129 (Compound 10b) is an effective, selective EGFR inhibitor with an IC50 of 51.2 nM and demonstrates broad-spectrum antiproliferative activity against the NCI tumor panel.

EGFR-IN-128 (compound 28) is a potent and selective molecule targeting wild-type EGFREx20Ins, demonstrating therapeutic efficacy across various human xenograft models and capable of penetrating the blood-brain barrier in preclinical species.

EGFR-IN-125 (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM for EGFR(d746-750 T790M C797S), 0.52 nM for EGFR(L858R T790M C797S), 0.5 nM for EGFR(d746-750 C797S), 0.69 nM for EGFR(L858R C797S), and 0.92 nM for EGFR (wild type).

EGFR-IN-120 (Compound 11eg) is an orally effective EGFR inhibitor. It exhibits potency against the EGFR L858R T790M C797S mutant with an IC50 of 0.053 μM, and displays weaker activity against EGFRWT, with an IC50 of 1.05 μM. EGFR-IN-120 inhibits the phosphorylation of EGFR as well as key downstream effectors including STAT3, AKT, and Erk. This compound induces cell cycle arrest and apoptosis in cells harboring the EGFR mutation. Additionally, EGFR-IN-120 inhibits the proliferation of NSCLC cells containing the EGFR L858R T790M C797S mutation, with an IC50 value of 0.052 μM.

EGFR-IN-121 (compound 15) acts as a dual inhibitor for EGFR and VEGFR-2, with IC50 values of 84 nM and 3.5 nM, respectively.

Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R T790M) and EGFR(L858R T790M C797S) inhibitor(IC50 of 12 nM and 13 nM, respectively. )

ZN-A-1041 is an inhibitor of HER2 in BT474 cells with an IC50 of 9.5 nM and wt-EGFR in H838 cells with an IC50 of 12 μM. It can be utilized for cancer and inflammation research [1].

Anticanceragent 231 (compound P5) is a tyrosine kinase inhibitor with an IC50 value of 3.95 μM. It targets the EGFR-ERK1 2 signaling pathway, reducing cell viability, proliferation, migration, and cancer stemness in triple-negative breast cancer (TNBC) cells, potentially playing a significant role in the treatment of TNBC.

Osimertinib-d6 is a deuterated compound of Osimertinib. Osimertinib has a CAS number of 1421373-65-0. Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small cell lung cancer (NSCLC).